JP2009542722A5 - - Google Patents
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- JP2009542722A5 JP2009542722A5 JP2009518635A JP2009518635A JP2009542722A5 JP 2009542722 A5 JP2009542722 A5 JP 2009542722A5 JP 2009518635 A JP2009518635 A JP 2009518635A JP 2009518635 A JP2009518635 A JP 2009518635A JP 2009542722 A5 JP2009542722 A5 JP 2009542722A5
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- JP
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- Prior art keywords
- alkyl
- compound according
- item
- cycloalkyl
- independently
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
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- 150000001875 compounds Chemical class 0.000 claims description 91
- -1 4-ethoxyphenyl Chemical group 0.000 claims description 63
- 125000004429 atoms Chemical group 0.000 claims description 21
- 125000000623 heterocyclic group Chemical group 0.000 claims description 18
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 17
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims description 12
- 125000004433 nitrogen atoms Chemical group N* 0.000 claims description 10
- 125000000719 pyrrolidinyl group Chemical group 0.000 claims description 10
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 claims description 9
- 125000003386 piperidinyl group Chemical group 0.000 claims description 9
- 125000000217 alkyl group Chemical group 0.000 claims description 8
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims description 8
- 229910052736 halogen Inorganic materials 0.000 claims description 8
- 150000002367 halogens Chemical class 0.000 claims description 8
- RWRDLPDLKQPQOW-UHFFFAOYSA-N pyrrolidine Chemical compound C1CCNC1 RWRDLPDLKQPQOW-UHFFFAOYSA-N 0.000 claims description 8
- 229910052731 fluorine Inorganic materials 0.000 claims description 7
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims description 6
- 230000001404 mediated Effects 0.000 claims description 6
- IJGRMHOSHXDMSA-UHFFFAOYSA-N nitrogen Substances N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims description 6
- 125000004043 oxo group Chemical group O=* 0.000 claims description 6
- 229910052757 nitrogen Inorganic materials 0.000 claims description 5
- 239000008194 pharmaceutical composition Substances 0.000 claims description 5
- 229920000728 polyester Polymers 0.000 claims description 5
- 125000006273 (C1-C3) alkyl group Chemical group 0.000 claims description 4
- 125000006570 (C5-C6) heteroaryl group Chemical group 0.000 claims description 4
- 239000003814 drug Substances 0.000 claims description 4
- 125000001153 fluoro group Chemical group F* 0.000 claims description 4
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims description 4
- 125000002757 morpholinyl group Chemical group 0.000 claims description 4
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims description 4
- NQRYJNQNLNOLGT-UHFFFAOYSA-N piperidine Chemical compound C1CCNCC1 NQRYJNQNLNOLGT-UHFFFAOYSA-N 0.000 claims description 4
- 150000003839 salts Chemical class 0.000 claims description 4
- 239000011780 sodium chloride Substances 0.000 claims description 4
- 125000004201 2,4-dichlorophenyl group Chemical group [H]C1=C([H])C(*)=C(Cl)C([H])=C1Cl 0.000 claims description 3
- 125000001255 4-fluorophenyl group Chemical group [H]C1=C([H])C(*)=C([H])C([H])=C1F 0.000 claims description 3
- 125000004172 4-methoxyphenyl group Chemical group [H]C1=C([H])C(OC([H])([H])[H])=C([H])C([H])=C1* 0.000 claims description 3
- 125000000590 4-methylphenyl group Chemical group [H]C1=C([H])C(=C([H])C([H])=C1*)C([H])([H])[H] 0.000 claims description 3
- 229910052794 bromium Inorganic materials 0.000 claims description 3
- 229910052801 chlorine Inorganic materials 0.000 claims description 3
- 238000004519 manufacturing process Methods 0.000 claims description 3
- 125000003854 p-chlorophenyl group Chemical group [H]C1=C([H])C(*)=C([H])C([H])=C1Cl 0.000 claims description 3
- 125000004182 2-chlorophenyl group Chemical group [H]C1=C([H])C(Cl)=C(*)C([H])=C1[H] 0.000 claims description 2
- 125000004189 3,4-dichlorophenyl group Chemical group [H]C1=C([H])C(Cl)=C(Cl)C([H])=C1* 0.000 claims description 2
- 125000004211 3,5-difluorophenyl group Chemical group [H]C1=C(F)C([H])=C(*)C([H])=C1F 0.000 claims description 2
- 125000004179 3-chlorophenyl group Chemical group [H]C1=C([H])C(*)=C([H])C(Cl)=C1[H] 0.000 claims description 2
- 125000004800 4-bromophenyl group Chemical group [H]C1=C([H])C(*)=C([H])C([H])=C1Br 0.000 claims description 2
- 125000004801 4-cyanophenyl group Chemical group [H]C1=C([H])C(C#N)=C([H])C([H])=C1* 0.000 claims description 2
- 125000004860 4-ethylphenyl group Chemical group [H]C1=C([H])C(=C([H])C([H])=C1*)C([H])([H])C([H])([H])[H] 0.000 claims description 2
- 125000004861 4-isopropyl phenyl group Chemical group [H]C1=C([H])C(=C([H])C([H])=C1*)C([H])(C([H])([H])[H])C([H])([H])[H] 0.000 claims description 2
- 125000004864 4-thiomethylphenyl group Chemical group 0.000 claims description 2
- 125000004863 4-trifluoromethoxyphenyl group Chemical group [H]C1=C([H])C(OC(F)(F)F)=C([H])C([H])=C1* 0.000 claims description 2
- 125000004199 4-trifluoromethylphenyl group Chemical group [H]C1=C([H])C(=C([H])C([H])=C1*)C(F)(F)F 0.000 claims description 2
- 125000004186 cyclopropylmethyl group Chemical group [H]C([H])(*)C1([H])C([H])([H])C1([H])[H] 0.000 claims description 2
- 229910052740 iodine Inorganic materials 0.000 claims description 2
- 125000003566 oxetanyl group Chemical group 0.000 claims description 2
- 125000003718 tetrahydrofuranyl group Chemical group 0.000 claims description 2
- 125000001412 tetrahydropyranyl group Chemical group 0.000 claims description 2
- 239000000203 mixture Substances 0.000 claims 2
- 238000002560 therapeutic procedure Methods 0.000 claims 1
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 description 12
- 201000010099 disease Diseases 0.000 description 8
- 0 C*(C)C([C@](*)(C(*)(*)*=C)C(*)(N(*)*)O*)=O Chemical compound C*(C)C([C@](*)(C(*)(*)*=C)C(*)(N(*)*)O*)=O 0.000 description 6
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 description 6
- 241000124008 Mammalia Species 0.000 description 4
- 125000002393 azetidinyl group Chemical group 0.000 description 3
- 125000004105 2-pyridyl group Chemical group N1=C([*])C([H])=C([H])C([H])=C1[H] 0.000 description 2
- 125000000113 cyclohexyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C([H])([H])C1([H])[H] 0.000 description 2
- 125000001511 cyclopentyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 description 2
- 230000002401 inhibitory effect Effects 0.000 description 2
- 125000003538 pentan-3-yl group Chemical group [H]C([H])([H])C([H])([H])C([H])(*)C([H])([H])C([H])([H])[H] 0.000 description 2
- 125000004193 piperazinyl group Chemical group 0.000 description 2
- 125000001436 propyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])[H] 0.000 description 2
- 125000000999 tert-butyl group Chemical group [H]C([H])([H])C(*)(C([H])([H])[H])C([H])([H])[H] 0.000 description 2
- 125000003349 3-pyridyl group Chemical group N1=C([H])C([*])=C([H])C([H])=C1[H] 0.000 description 1
- 125000000339 4-pyridyl group Chemical group N1=C([H])C([H])=C([*])C([H])=C1[H] 0.000 description 1
- UYDLXPVUXCQPMP-GOSISDBHSA-N CC([C@@H](Cc(cc1)ccc1OCc1ccccc1)NC)=O Chemical compound CC([C@@H](Cc(cc1)ccc1OCc1ccccc1)NC)=O UYDLXPVUXCQPMP-GOSISDBHSA-N 0.000 description 1
- IISJSOKHDDJFJD-JTQLQIEISA-N CC([C@H](Cc(cc1)ccc1Cl)N)=O Chemical compound CC([C@H](Cc(cc1)ccc1Cl)N)=O IISJSOKHDDJFJD-JTQLQIEISA-N 0.000 description 1
- MHPCUBVYJYHDEA-UHFFFAOYSA-N CNC(C(Cc(cc1F)ccc1Cl)CN)=O Chemical compound CNC(C(Cc(cc1F)ccc1Cl)CN)=O MHPCUBVYJYHDEA-UHFFFAOYSA-N 0.000 description 1
- SMVSJSSXYMNJBS-SECBINFHSA-N COc1ccc(C[C@H](C(N)=O)N)cc1 Chemical compound COc1ccc(C[C@H](C(N)=O)N)cc1 SMVSJSSXYMNJBS-SECBINFHSA-N 0.000 description 1
- 208000008787 Cardiovascular Disease Diseases 0.000 description 1
- JLSKPBDKNIXMBS-SECBINFHSA-N N[C@H](Cc1c[nH]c2c1cccc2)C(N)=O Chemical compound N[C@H](Cc1c[nH]c2c1cccc2)C(N)=O JLSKPBDKNIXMBS-SECBINFHSA-N 0.000 description 1
- 206010053643 Neurodegenerative disease Diseases 0.000 description 1
- 230000003463 hyperproliferative Effects 0.000 description 1
- 200000000018 inflammatory disease Diseases 0.000 description 1
- 125000000959 isobutyl group Chemical group [H]C([H])([H])C([H])(C([H])([H])[H])C([H])([H])* 0.000 description 1
- 239000003909 protein kinase inhibitor Substances 0.000 description 1
Applications Claiming Priority (3)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US81895206P | 2006-07-06 | 2006-07-06 | |
US60/818,952 | 2006-07-06 | ||
PCT/US2007/072884 WO2008006039A1 (en) | 2006-07-06 | 2007-07-05 | Dihydrothieno pyrimidines as akt protein kinase inhibitors |
Publications (3)
Publication Number | Publication Date |
---|---|
JP2009542722A JP2009542722A (ja) | 2009-12-03 |
JP2009542722A5 true JP2009542722A5 (es) | 2011-08-11 |
JP5231411B2 JP5231411B2 (ja) | 2013-07-10 |
Family
ID=38631534
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
JP2009518635A Active JP5231411B2 (ja) | 2006-07-06 | 2007-07-05 | Aktプロテインキナーゼ阻害剤としてのジヒドロチエノピリミジン |
Country Status (9)
Country | Link |
---|---|
US (1) | US9303040B2 (es) |
EP (1) | EP2054418B1 (es) |
JP (1) | JP5231411B2 (es) |
CN (1) | CN101516891B (es) |
AT (1) | ATE532789T1 (es) |
CA (1) | CA2656364C (es) |
DK (1) | DK2054418T3 (es) |
SI (1) | SI2054418T1 (es) |
WO (1) | WO2008006039A1 (es) |
Families Citing this family (18)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
UA95641C2 (en) * | 2006-07-06 | 2011-08-25 | Эррей Биофарма Инк. | Hydroxylated cyclopenta [d] pyrimidines as akt protein kinase inhibitors |
DE602007011628D1 (de) * | 2006-07-06 | 2011-02-10 | Array Biopharma Inc | Dihydrofuropyrimidine als akt-proteinkinaseinhibitoren |
EP2054418B1 (en) * | 2006-07-06 | 2011-11-09 | Array Biopharma Inc. | Dihydrothieno pyrimidines as akt protein kinase inhibitors |
US8063050B2 (en) | 2006-07-06 | 2011-11-22 | Array Biopharma Inc. | Hydroxylated and methoxylated pyrimidyl cyclopentanes as AKT protein kinase inhibitors |
US9409886B2 (en) | 2007-07-05 | 2016-08-09 | Array Biopharma Inc. | Pyrimidyl cyclopentanes as AKT protein kinase inhibitors |
US8846683B2 (en) | 2007-07-05 | 2014-09-30 | Array Biopharma, Inc. | Pyrimidyl cyclopentanes as Akt protein kinase inhibitors |
WO2009089352A1 (en) | 2008-01-08 | 2009-07-16 | Array Biopharma Inc. | Pyrrolopyridines as kinase inhibitors |
WO2009089359A1 (en) | 2008-01-09 | 2009-07-16 | Array Biopharma Inc. | Pyrazolopyridines as kinase inhibitors |
JP5539225B2 (ja) | 2008-01-09 | 2014-07-02 | アレイ バイオファーマ、インコーポレイテッド | Aktタンパク質キナーゼ阻害剤としての水酸化されたピリミジルシクロペンタン |
ES2426092T3 (es) | 2008-01-09 | 2013-10-21 | Array Biopharma, Inc. | 5H-Ciclopenta[d]pirimidinas como inhibidores de proteínas cinasas AKT |
DE102010025663A1 (de) * | 2010-06-30 | 2012-01-05 | Karl-Heinz Glüsenkamp | Neue beta-Aminoaldehyd-Derivate, Verfahren zu ihrer Herstellung und ihre chemische Verwendung als reaktive Intermediate |
EP2694072B1 (en) | 2011-04-01 | 2017-11-29 | Genentech, Inc. | Combination of akt inhibitor compound and abiraterone for use in therapeutic treatments |
MX2013011333A (es) | 2011-04-01 | 2014-04-16 | Genentech Inc | Combinaciones de compuestos inhibidores de akt y mek, y metodos de uso. |
US20160264568A1 (en) * | 2013-06-07 | 2016-09-15 | Bayer Pharma Aktiengesellschaft | Substituted triazolopyridines having activity as mps-1 inhibitors |
JP6405190B2 (ja) | 2014-10-10 | 2018-10-17 | 株式会社コスメック | 出力装置 |
WO2017102378A1 (en) | 2015-12-14 | 2017-06-22 | Asml Netherlands B.V. | A membrane assembly |
US10722484B2 (en) | 2016-03-09 | 2020-07-28 | K-Gen, Inc. | Methods of cancer treatment |
CN113087718B (zh) * | 2020-01-09 | 2024-02-09 | 四川科伦博泰生物医药股份有限公司 | 噻吩并嘧啶酮类化合物及其医药应用 |
Family Cites Families (91)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US3885035A (en) | 1972-04-05 | 1975-05-20 | Sandoz Ag | Method for treating arrhythmia by using 1,4-bis(4 quinazolinyl) piperazines |
US3956495A (en) | 1973-10-30 | 1976-05-11 | Eli Lilly And Company | 2,4-Diaminoquinazolines as antithrombotic agents |
US3966936A (en) | 1974-02-21 | 1976-06-29 | Pfizer Inc. | Piperazino quinazoline bronchodilators |
US4060615A (en) | 1976-02-18 | 1977-11-29 | Mead Johnson & Company | 2-Piperazinyl-6,7-dimethoxyquinazolines |
JPS562968A (en) | 1979-06-21 | 1981-01-13 | Mitsubishi Yuka Yakuhin Kk | Novel pyrimidine derivative |
US4749704A (en) | 1985-03-07 | 1988-06-07 | Sankyo Company Limited | Cyclopenta[d]pyrimidine derivatives and use as antidepressants |
EP0799617A3 (en) | 1986-02-24 | 1997-11-12 | Mitsui Petrochemical Industries, Ltd. | Therapeutic agent for neurological diseases |
US4889856A (en) | 1987-08-31 | 1989-12-26 | Merck & Co., Inc. | 7,8-dihydro-4-(1-pierazinyl)-6H-thiopyrano-[3,2-d] pyrimidines as β-blockers |
US4871739A (en) | 1987-01-21 | 1989-10-03 | Merck & Co., Inc. | Substituted 6H-7,8-dihydrothiapyrano(3,2-D)-pyrimidines as hyopglycemic agents |
US4994464A (en) | 1987-08-31 | 1991-02-19 | Merck & Co., Inc. | Piperazinylpyrimidines as β-adrenergic receptor blockers |
MX19185A (es) | 1989-01-20 | 1993-12-01 | Pfizer | Procedimiento para preparar 3-(1,2,5,6-tretrahidropiridil)-pirrolopiridinas. |
DE69329067T2 (de) | 1992-10-05 | 2001-05-10 | Ube Industries | Pyridmidin-derivate |
WO1995003286A1 (fr) | 1993-07-23 | 1995-02-02 | The Green Cross Corporation | Derive de triazole et son utilisation pharmaceutique |
GB9416189D0 (en) | 1994-08-10 | 1994-09-28 | Merck Sharp & Dohme | Therapeutic agents |
DE69530989T2 (de) | 1994-08-13 | 2004-05-19 | Yuhan Corp. | Neue pyrimidinderivate und verfahren zu ihrer herstellung |
US5525625A (en) | 1995-01-24 | 1996-06-11 | Warner-Lambert Company | 2-(2-Amino-3-methoxyphenyl)-4-oxo-4H-[1]benzopyran for treating proliferative disorders |
US7067664B1 (en) | 1995-06-06 | 2006-06-27 | Pfizer Inc. | Corticotropin releasing factor antagonists |
ZA979961B (en) | 1996-11-15 | 1999-05-05 | Lilly Co Eli | 5-HT1F agonists |
UA73073C2 (uk) | 1997-04-03 | 2005-06-15 | Уайт Холдінгз Корпорейшн | Заміщені 3-ціанохіноліни, спосіб їх одержання та фармацевтична композиція |
US6506798B1 (en) | 1997-07-01 | 2003-01-14 | Warner-Lambert Company | 4-Arylamino, 4-aryloxy, and 4-arylthio diarylamines and derivatives thereof as selective MEK inhibitors |
ATE277895T1 (de) | 1997-07-01 | 2004-10-15 | Warner Lambert Co | 4-brom or 4-iod-phenylamino- benzhydroxamsäurederivate und ihre anwendung als mek-inhibitoren |
KR20010014360A (ko) | 1997-07-01 | 2001-02-26 | 로즈 암스트롱, 크리스틴 에이. 트러트웨인 | 2-(4-브로모 또는 4-요오도 페닐아미노)벤조산 유도체 및mek 억제제로서의 그의 용도 |
US6821963B2 (en) | 1997-07-01 | 2004-11-23 | Warner-Lambert Company | 4-Bromo or 4-iodo phenylamino benzhydroxamic acid derivatives and their use as MEK inhibitors |
US6310060B1 (en) | 1998-06-24 | 2001-10-30 | Warner-Lambert Company | 2-(4-bromo or 4-iodo phenylamino) benzoic acid derivatives and their use as MEK inhibitors |
ATE496035T1 (de) | 1998-03-31 | 2011-02-15 | Kyowa Hakko Kirin Co Ltd | Stickstoffenthaltende heterocyclische verbindungen |
DE19853278A1 (de) | 1998-11-19 | 2000-05-25 | Aventis Pharma Gmbh | Substituierte 4-Amino-2-aryl-cyclopenta[d]pyrimidine, ihre Herstellung, ihre Verwendung und sie enthaltende pharmazeutische Präparate |
US6696440B1 (en) | 1999-01-07 | 2004-02-24 | Warner-Lambert Company | Treatment of asthma with MEK inhibitors |
WO2000040237A1 (en) | 1999-01-07 | 2000-07-13 | Warner-Lambert Company | Antiviral method using mek inhibitors |
KR20010108093A (ko) | 1999-01-13 | 2001-12-07 | 로즈 암스트롱, 크리스틴 에이. 트러트웨인 | 1-헤테로고리 치환된 디아릴아민 |
JP2002534446A (ja) | 1999-01-13 | 2002-10-15 | ワーナー−ランバート・カンパニー | 4′ヘテロアリールジアリールアミン |
WO2000042003A1 (en) | 1999-01-13 | 2000-07-20 | Warner-Lambert Company | Benzenesulfonamide derivatives and their use as mek inhibitors |
CA2348236A1 (en) | 1999-01-13 | 2000-07-20 | Stephen Douglas Barrett | 4-arylamino, 4-aryloxy, and 4-arylthio diarylamines and derivatives thereof as selective mek inhibitors |
AU2482800A (en) | 1999-01-13 | 2000-08-01 | Warner-Lambert Company | Sulphohydroxamic acids and sulphohydroxamates and their use as mek inhibitors |
CA2355470C (en) | 1999-01-13 | 2008-09-30 | Warner-Lambert Company | Benzoheterocycles and their use as mek inhibitors |
GB9910577D0 (en) | 1999-05-08 | 1999-07-07 | Zeneca Ltd | Chemical compounds |
IL147618A0 (en) | 1999-07-16 | 2002-08-14 | Warner Lambert Co | Method for treating chronic pain using mek inhibitors |
HUP0202319A3 (en) | 1999-07-16 | 2004-12-28 | Warner Lambert Co | Use of mek inhibitors for the preparation of pharmaceutical compositions treating chronic pain |
CA2377100A1 (en) | 1999-07-16 | 2001-01-25 | Warner-Lambert Company | Method for treating chronic pain using mek inhibitors |
CA2374052A1 (en) | 1999-07-16 | 2001-01-25 | Warner-Lambert Company | Method for treating chronic pain using mek inhibitors |
JP2003527379A (ja) | 2000-03-15 | 2003-09-16 | ワーナー−ランバート・カンパニー、リミテッド、ライアビリティ、カンパニー | Mex阻害物質としての5−アミド置換ジアリールアミン類 |
US6960614B2 (en) | 2000-07-19 | 2005-11-01 | Warner-Lambert Company | Oxygenated esters of 4-lodo phenylamino benzhydroxamic acids |
BR0113520A (pt) | 2000-08-25 | 2003-06-24 | Warner Lambert Co | Processo de preparação de ácidos n-aril-antranìlicos e seus derivados |
US7067532B2 (en) | 2000-11-02 | 2006-06-27 | Astrazeneca | Substituted quinolines as antitumor agents |
HUP0401544A2 (hu) * | 2001-03-02 | 2004-12-28 | Bristol-Myers Squibb Company | Melanokortin receptor modulátoraiként hasznos vegyületek és a vegyületeket tartalmazó gyógyszerkészítmények |
WO2002083139A1 (en) | 2001-04-10 | 2002-10-24 | Merck & Co., Inc. | Inhibitors of akt activity |
US7279474B2 (en) | 2001-04-30 | 2007-10-09 | Glaxo Group Limited | Substituted pyrrolo[2,3-d]pyrimidines as antagonists of the corticotropin releasing factor (CRF) |
US7115741B2 (en) | 2001-09-06 | 2006-10-03 | Levy Daniel E | 4-thieno[2,3-D]pyrimidin-4-YL piperazine compounds |
US20030187026A1 (en) | 2001-12-13 | 2003-10-02 | Qun Li | Kinase inhibitors |
TW200306819A (en) | 2002-01-25 | 2003-12-01 | Vertex Pharma | Indazole compounds useful as protein kinase inhibitors |
CA2478534A1 (en) | 2002-03-13 | 2003-09-25 | Array Biopharma, Inc. | N3 alkylated benzimidazole derivatives as mek inhibitors |
ES2407849T3 (es) | 2002-03-13 | 2013-06-14 | Array Biopharma, Inc. | Derivados de bencimidazol alquilados N3 como inhibidores de MEK |
US7235537B2 (en) | 2002-03-13 | 2007-06-26 | Array Biopharma, Inc. | N3 alkylated benzimidazole derivatives as MEK inhibitors |
US7223738B2 (en) | 2002-04-08 | 2007-05-29 | Merck & Co., Inc. | Inhibitors of Akt activity |
JP4451136B2 (ja) | 2002-04-08 | 2010-04-14 | メルク エンド カムパニー インコーポレーテッド | Akt活性阻害薬 |
AU2003226250B2 (en) | 2002-04-08 | 2007-08-16 | Merck Sharp & Dohme Corp. | Inhibitors of Akt activity |
EP1494676B1 (en) | 2002-04-08 | 2013-05-08 | Merck Sharp & Dohme Corp. | Fused quinoxaline derivatives as inhibitors of akt activity |
AU2003230367A1 (en) | 2002-05-10 | 2003-11-11 | Neurocrine Biosciences, Inc. | Substituted piperazine as melanocortin receptors ligands |
US20040102360A1 (en) | 2002-10-30 | 2004-05-27 | Barnett Stanley F. | Combination therapy |
JP2006507299A (ja) | 2002-10-30 | 2006-03-02 | メルク エンド カムパニー インコーポレーテッド | Akt活性の阻害薬 |
GB0308208D0 (en) | 2003-04-09 | 2003-05-14 | Glaxo Group Ltd | Chemical compounds |
AU2004233827B2 (en) | 2003-04-24 | 2009-05-28 | Merck Sharp & Dohme Corp. | Inhibitors of Akt activity |
EP1646615B1 (en) | 2003-06-06 | 2009-08-26 | Vertex Pharmaceuticals Incorporated | Pyrimidine derivatives as modulators of atp-binding cassette transporters |
MXPA06001494A (es) | 2003-08-05 | 2007-05-11 | Vertex Pharma | Compuestos de piramidina condensados como inhibidores de canales ionicos gatillados por tension. |
JP2007501821A (ja) | 2003-08-12 | 2007-02-01 | エフ.ホフマン−ラ ロシュ アーゲー | Cfrアンタゴニストとしてのテトラヒドロキナゾリン誘導体 |
AU2004272437A1 (en) | 2003-09-09 | 2005-03-24 | Ono Pharmaceutical Co., Ltd. | CRF antagonists and heterobicyclic compounds |
WO2005039564A1 (en) | 2003-10-02 | 2005-05-06 | Vertex Pharmaceuticals Incorporated | Phthalimide compounds useful as protein kinase inhibitors |
CN102786482A (zh) | 2003-11-21 | 2012-11-21 | 阿雷生物药品公司 | Akt蛋白激酶抑制剂 |
US8076338B2 (en) | 2004-04-23 | 2011-12-13 | Exelixis, Inc. | Kinase modulators and methods of use |
US20060025074A1 (en) | 2004-07-30 | 2006-02-02 | Chih-Ming Liang | Bluetooth-based headset |
AU2005281704A1 (en) | 2004-09-06 | 2006-03-16 | Nycomed Gmbh | Novel pyrazolopyrimidines |
TWM266655U (en) | 2004-09-23 | 2005-06-01 | Blueexpert Technology Corp | Bluetooth earphone device capable of wirelessly receiving and transmitting stereo sound signal and digital information signal |
TW200621257A (en) * | 2004-10-20 | 2006-07-01 | Astellas Pharma Inc | Pyrimidine derivative fused with nonaromatic ring |
UY29177A1 (es) | 2004-10-25 | 2006-05-31 | Astex Therapeutics Ltd | Derivados sustituidos de purina, purinona y deazapurina, composiciones que los contienen métodos para su preparación y sus usos |
WO2006071819A1 (en) | 2004-12-28 | 2006-07-06 | Exelixis, Inc. | [1h-pyrazolo[3, 4-d]pyrimidin-4-yl]-piperidine or -piperazine compounds as serine-theoronine kinase modulators (p70s6k, atk1 and atk2) for the treatment of immunological, inflammatory and proliferative diseases |
CA2598956A1 (en) | 2005-02-24 | 2006-08-31 | Pfizer Products Inc. | Bicyclic heteroaromatic derivatives useful as anticancer agents |
EP1881983B1 (en) | 2005-05-20 | 2012-01-11 | Vertex Pharmaceuticals, Inc. | Pyrrolopyridines useful as inhibitors of protein kinase |
UY29610A1 (es) | 2005-06-21 | 2007-01-31 | Cancer Rec Tech Ltd | Aril-alquilaminas y heteroaril-alquilaminas como inhibidores de la quinasa proteínica |
PE20070593A1 (es) | 2005-10-13 | 2007-07-23 | Glaxo Group Ltd | Compuestos pirrolopirimidina como inhibidores de syk |
PE20071164A1 (es) | 2005-12-28 | 2008-01-11 | Takeda Pharmaceutical | Compuestos heterociclico fusionado como antagonista del receptor mineralocorticoide |
US20090124610A1 (en) | 2006-04-25 | 2009-05-14 | Gordon Saxty | Pharmaceutical compounds |
RU2008152171A (ru) | 2006-07-05 | 2010-08-10 | Интермьюн, Инк. (Us) | Новые ингибиторы вирусной репликации гепатита с |
US8063050B2 (en) | 2006-07-06 | 2011-11-22 | Array Biopharma Inc. | Hydroxylated and methoxylated pyrimidyl cyclopentanes as AKT protein kinase inhibitors |
UA95641C2 (en) * | 2006-07-06 | 2011-08-25 | Эррей Биофарма Инк. | Hydroxylated cyclopenta [d] pyrimidines as akt protein kinase inhibitors |
EP2054418B1 (en) * | 2006-07-06 | 2011-11-09 | Array Biopharma Inc. | Dihydrothieno pyrimidines as akt protein kinase inhibitors |
US7910747B2 (en) | 2006-07-06 | 2011-03-22 | Bristol-Myers Squibb Company | Phosphonate and phosphinate pyrazolylamide glucokinase activators |
GB0613518D0 (en) | 2006-07-06 | 2006-08-16 | Phytopharm Plc | Chemical compounds |
RU2481336C2 (ru) | 2006-07-06 | 2013-05-10 | Эррэй Биофарма Инк. | Циклопента(d)пиримидины в качестве ингибиторов протеинкиназ акт |
TW200808325A (en) | 2006-07-06 | 2008-02-16 | Astrazeneca Ab | Novel compounds |
PL2049478T3 (pl) | 2006-07-06 | 2012-09-28 | Glaxo Group Ltd | Podstawione N-fenylometylo 5-okso-prolino-2-amidy jako antagoniści receptora P2X7 oraz sposoby ich zastosowania |
DE602007011628D1 (de) * | 2006-07-06 | 2011-02-10 | Array Biopharma Inc | Dihydrofuropyrimidine als akt-proteinkinaseinhibitoren |
WO2008012635A2 (en) | 2006-07-26 | 2008-01-31 | Pfizer Products Inc. | Amine derivatives useful as anticancer agents |
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